2016年9月23日星期五

Agomelatine


Agomelatine (BAN, rINN; trade names Valdoxan, Melitor, Thymanax) is a melatonergic antidepressant developed by the pharmaceutical company Servier. It is marketed for the treatment of major depressive disorder, primarily for its relatively favorable side effect profile: it avoids the weight gain, sexual dysfunction, and severe withdrawal associated with the most commonly used classes of antidepressants (SSRIs, SNRIs, tricyclics), while providing similar therapeutic benefit.

Due to its distinctive mechanism of action, agomelatine is also studied for its effects on sleep regulation. Studies report various improvements in general quality of sleep metrics, as well as specific therapeutic benefits in circadian rhythm disorders.

Medical uses

Major depressive disorder

Agomelatine is indicated for the treatment of major depressive episodes in adults. Ten placebo controlled trials have been performed to investigate the short term efficacy of agomelatine in major depressive disorder. At the end of treatment, significant efficacy was demonstrated in six of the ten short-term double-blind placebo-controlled studies. Two were considered "failed" trials, as comparators of established efficacy failed to differentiate from placebo. Efficacy was also observed in more severely depressed patients in all positive placebo-controlled studies.The maintenance of antidepressant efficacy was demonstrated in a relapse prevention study. A large meta-analysis of 20 trials with 7460 participants found agomelatine to be as effective as standard antidepressants.

Results of the meta-analysis of three positive, randomized, double-blind, placebo controlled studies in 357 patients treated with agomelatine and 360 patients treated with placebo show that agomelatine is effective in treating severe depression. Its antidepressant effect is greater for more severe depression. In patients with a greater baseline score (>30 on HAMD17 scale), the agomelatine-placebo difference was of 4.53 points.Controlled studies in humans have shown that agomelatine is at least as effective as the SSRI antidepressants paroxetine, sertraline, escitalopram, and fluoxetine in the treatment of major depression.

A small open-label study has suggested efficacy in the treatment of atypical and melancholic depression. Well-designed clinical trials have demonstrated efficacy in the treatment of anxious depression.Agomelatine’s onset of action has been reported to occur as early as the first week of treatment.

However, the body of research on agomelatine has been substantially affected by publication bias, prompting analyses which take into account both published and unpublished studies. These have confirmed that agomelatine is (statistically) approximately as effective as more commonly used antidepressants (eg SSRIs), but some qualified this as "marginally clinically relevant",being only slightly above placebo.

Investigational

Additionally, possibly because of its action on melatonin receptors, agomelatine appears to improve sleep quality, with no reported daytime drowsiness. Agomelatine has demonstrated anxiolytic properties in rodents. It has been found significantly more effective than placebo in the treatment of generalised anxiety disorder. There is tentative evidence to suggest the efficacy of agomelatine as either a monotherapy or adjunct in the treatment of obsessive-compulsive disorder (OCD). A case report documenting the efficacy of agomelatine in the treatment of social anxiety disorder has been published. An open-label study has found agomelatine to be efficacious in the treatment of seasonal affective disorder. Open-label studies have suggested efficacy of adjunctive agomelatine in bipolar depression. A study in mice found that it protected against pentylenetetrazole- and pilocarpine-induced seizures. A small placebo-controlled trial found some benefit of agomelatine in attention deficit hyperactivity disorder (ADHD).

Use in special populations

It is not recommended for use in children and adolescents below 18 years of age due to a lack of data on safety and efficacy. Only limited clinical data is available on the use of agomelatine in elderly patients ≥ 65 years old with major depressive episodes. Therefore, caution should be exercised when prescribing it to these patients.


Introduction: 
Place of orgin : China
Specifications:
CAS no. : 138112-76-2
Molecular formula: C12H18N4O5S
Molecular weight: 330.3601
Storage :Store in cool and dry palce. Keep away from strong light ,high temperature.
Usage: Used for Melatonin hormonal drugs
transportation:by express delivery (by EMS,DHL,TNT & FEDEX) or sea & air shipping.
Shipment term: EXW, FOB, CIF, CNF
Sample: At any time to provide (lowest price & highest quality)

Specifications:

ItemsSpecificationsResults
Appearance White to almost white crystalline powderwhite crystalline powder
SolubilityThis product is soluble in DMF, methanol, ethanol, water and 0.1mol/L hydrochloric acid solution almost not.108.4-108.5°C
Identification  
UVHas an absorption maximum at 230nmConforms
IRCorresponding to reference spectrumConforms
HPLCShould the retention time of the main peak of the reference solutionConforms
Examination  
Chloride≤0.01%Conforms
Related substances  
Single impurity≤0.5%0.049%
Total impurity≤0.1%0.06%
Impurities I≤0.1%Not detected
Impurities II≤0.1%Not detected
Residual solvent  
N-hexane≤0.029%0.0002%
Ethanol≤0.5%0.1%
Dichloromethane≤0.06%Not detected
Ethyl acetate≤0.5%Not detected
Tetrahydrofuran≤0.072%Not detected
Toluene≤0.089%Not detected
Chloroform≤0.006%0.001%
Loss on drying≤0.5%0.002%
Residue on ignition≤0.1%0.06%
Heavy metal≤20ppmConforms
Assay≥99.0%99.52%
Conclusion:Qualified


Packaging & Shipping: 

 25kg/drum,1kg/bag or according to customer request 
Transit could be DHL,UPS,TNT,EMS,Fedex,and so on.

For mass orders, it will be delivered by air or sea

my contact infomation is:

Email: cloris_2016@tuskwei.com or

bettytuskwei@yahoo.com

Skype: betty_3451

Website: http://www.tuskwei.net/

Notice: This product is only suitable for laboratory use, or the use of animals. It can not be used directly on the human body

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